Aminoketone derivatives of 1,2-oxazole and use thereof

Details Aminoketone derivatives of 1,2-oxazole and use thereof Aminoketone derivatives of 1,2-oxazole and use thereof

1992-02-24

1994-08-16

Springer, David B.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

540 3, 540207, C07D41306, A61K 3142

Patent

active

053388577

ABSTRACT:
Aminoketone derivative compounds containing a heterocyclic ring bonded to an aminoketone moiety and useful as effective ingredients of centrally acting muscle relaxants and pollakiurea curing agents.
(+)3-phenyl-5-[2-(1-pyrrolidinylmethyl)butyryl]isoxazole, which has a more remarkable central muscle relaxant action as compared with its racemic modification, can be effectively separated from the racemic modification using optically active 10-camphorsulfonic acid as the agent for the optical resolution.

REFERENCES:
European Search Report of 9230 1510 (European equivalent).
"The Merck Index", 11th Edition, 1989, p. 262, edited by S. Budavari et al. Merck & Co., Inc. Rahway, US.
Journal of Organic Chemistry, vol. 52, No. 25, Dec. 11, 1987, pp. 5501-5505 US; R. R. Sauers et al., "Synthesis and Photochemistry of Heterocyclic Norbornenyl Ketones", p. 5504.
Chemical Abstracts, vol. 102, No. 11, Mar. 18, 1985, p. 574, Abstract No. 95628x, Columbus, Ohio, US; JP-A-59181267 (Nippon Kayaku Co., Ltd.).
Chemical and Pharmaceutical Bulletin, vol. 34, No. 4, 1986, pp. 1643-1655; T. Tatee et al.: "Isoxazole Derivatives as Centrally Acting Muscle Relaxants II. Synthesis and Structure-Activity Relationship of 3-Amino-N-(3-phenyl-5-isoxazolyl) propanamides", p. 1646.

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